GRADE & PURITY 10mM in DMSO

Synonyms

8-Azaspiro[4.5]decane-7,9-dione, 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-, hydrochloride (1:2)

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

BMY 7378 is a multi-targeted inhibitor ofα2C-adrenoceptorandα1D-adrenoceptorwithpKiof 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for5-HT1Areceptor withpKiof 8.3.
In vitro

BMY 7378 shows 10-fold selectivity for α_2C-adrenoceptors over other α₂-adrenoceptors with pKi of 6.54. BMY 7378 is selective for the α_1D-adrenoceptor subtype (PKi: hamster α_1b-adrenoceptor 6.2, human α_1b-adrenoceptor 7.2; bovine α_1c-adrenoceptor 6.1, human α_1c-adrenoceptor 6.6; rat α_1d-adrenoceptor 8.2, human α_1d-adrenoceptor 9.4 BMY 7378 at concentration of 1 nM to 30 nM elicits inhibitory effects in a concentration-dependent manner in the rat dorsal raphe nucleus.

In vivo

BMY 7378 (pA₂ of 8.67) is approximately 100 times more potent than yohimbine (pA₂ of 6.62) against contractions to noradrenaline in rat aorta. BMY 7378 (pA₂ of 6.48) is approximately 10 times less potent than yohimbine (pA₂ of 7.56) at antagonizing the contractile response to noradrenaline in human saphenous vein (α_2C-adrenoceptor). BMY 7378 dose dependently (0.25-5 mg/kg s.c.) reduces the undetectable levels forepaw treading and head weaving induced by 8-OH-DPAT (0.75 mg/kg s.c.) in rats. BMY 7378 causes a marked and dose-dependent (0.01-1.0 mg/kg s.c.) decrease of 5-HT release in ventral hippocampus of the anaesthetized rat as detected by brain microdialysis in rats.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

8-Azaspiro[4.5]decane-7, 9-dione, 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-, hydrochloride (1:2)

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pK_i of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pK_i of 8.3.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

AGONIST

Nombres e identificadores

• Isómeros SMILES: COC1=CC=CC=C1N2CCN(CC2)CCN3C(=O)CC4(CCCC4)CC3=O.Cl.Cl
• WGK Alemania: 3
• RTECS: GY3996000
• PubChem CID: 210172
• Peso molecular: 458.42

Objetivos asociados (humanos)

ADRA1B Tclin Alpha-1B adrenergic receptor (1 Activities)

Discover Target: ADRA1B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA1D Tclin Alpha-1D adrenergic receptor (3 Activities)

Discover Target: ADRA1D

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA1A Tclin Alpha-1A adrenergic receptor (1 Activities)

Discover Target: ADRA1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR1A Tclin 5-hydroxytryptamine receptor 1A (2 Activities)

Discover Target: HTR1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 33 mg/mL (198.59 mM); Ethanol: 33 mg/mL (198.59 mM); Water: Insoluble
• Punto de fusión (°C): 196.5-198.5°C